3-nitro-2-[(R)-(tetrahydro-pyran-3-yl)oxy]-pyridine | 1332712-65-8

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 3-nitro-2-[(R)-(tetrahydro-pyran-3-yl)oxy]-pyridine
• 英文别名: 3-nitro-2-[(3R)-oxan-3-yl]oxypyridine
• CAS: 1332712-65-8
• 化学式: C₁₀H₁₂N₂O₄
• 分子量: 224.216
• InChiKey: PNWGYIAXNDWHPF-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  77.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-氟-3-硝基吡啶 、 四氢吡喃-3(R)-环醇 生成 3-nitro-2-[(R)-(tetrahydro-pyran-3-yl)oxy]-pyridine
  参考文献：
  名称：

  HETEROCYCLOALKYL-CONTAINING THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS

  摘要：

  本发明涉及包含噻吩嘧啶化合物的新型药物组合物。此外，本发明还涉及使用本发明中的噻吩嘧啶化合物制备用于预防和/或治疗可以通过抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b）激酶活性影响的疾病的药物组合物。

  公开号：

  US20110212102A1

文献信息

• [EN] HETEROCYCLOALKYL-CONTAINING THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS<br/>[FR] THIÉNOPYRIMIDINES CONTENANT UN GROUPE HÉTÉROCYCLOALKYLE POUR DES COMPOSITIONS PHARMACEUTIQUES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2011104337A1

  公开（公告）日：2011-09-01

  The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

  本发明涉及包含噻吩并嘧啶化合物的新颖药物组合物。此外，本发明涉及利用本发明的噻吩并嘧啶化合物生产药物组合物，用于预防和/或治疗可通过抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b）及其变体的激酶活性而影响的疾病。
• [EN] NEW 6-MEMBERED HETEROAROMATIC SUBSTITUTED CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE CYANOINDOLINE À SUBSTITUTION HÉTÉROAROMATIQUE À 6 CHAÎNONS UTILISÉS COMME INHIBITEURS DE NIK
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2017125534A1

  公开（公告）日：2017-07-27

  The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

  本发明涉及公式（I）的药物制剂，用于治疗和/或预防哺乳动物，特别是用于治疗癌症、炎症性疾病、代谢性疾病和自身免疫性疾病的NF-KB诱导激酶（NIK - 也称为MAP3K14）抑制剂。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物或药物组合物预防或治疗癌症、炎症性疾病、包括肥胖和糖尿病在内的代谢性疾病以及自身免疫性疾病的用途。
• Heterocycloalkyl-containing thienopyrimidines for pharmaceutical compositions
  申请人：Lehmann-Lintz Thorsten

  公开号：US08648068B2

  公开（公告）日：2014-02-11

  The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

  本发明涉及新型药物组合物，其中包含噻唑嘧啶化合物。此外，本发明还涉及使用本发明中的噻唑嘧啶化合物生产药物组合物，用于预防和/或治疗可以受到Mnk1和/或Mnk2（Mnk2a或Mnk2b）及/或其变体的激酶活性抑制影响的疾病。
• 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
  申请人：Janssen Pharmaceutica NV

  公开号：US11001569B2

  公开（公告）日：2021-05-11

  The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as a cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

  本发明涉及式(I)的药物制剂，可用于哺乳动物的治疗和/或预防，尤其涉及NF-κB诱导激酶（NIK-又称MAP3K14）的抑制剂，可用于治疗癌症、炎症性疾病、代谢性疾病和自身免疫性疾病等疾病。本发明还涉及包含此类化合物的药物组合物，以及使用此类化合物或药物组合物预防或治疗癌症、炎症性疾病、代谢紊乱（包括肥胖和糖尿病）和自身免疫性疾病等疾病。
• 4-[HETEROCYCLOALKYLOXY(HETERO)ARYLAMINO] THIENO[2,3-D]PYRIMIDINES HAVING MNK1/ MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2539346B1

  公开（公告）日：2014-04-16